Sodium-dependent glucose cotransporters (“SGLTs”) are a family of glucose transporters.
Research shows that more than 99% of renal glucose is resorbed by two subtypes of SGLTs, i.e. SGLT1 and SGLT2. More specifically, about 10% of renal glucose reabsorption is accomplished by low-capacity, high affinity SGLT1, which is mainly expressed in the small intestine and the S3 segment of the kidney's proximal tubule; and about 90% of renal glucose reabsorption is mediated by high-capacity, low affinity SGLT2, which is found in the 51 segment of the kidney's proximal tubule. Inhibiting SGLT2 activities results in suppression of renal glucose reabsorption, thereby decreasing blood sugar level.
A number of SGLT2 inhibitors have been discovered. They have potentials to be used as anti-diabetic drugs. See e.g., Han et al., Diabetes, 2008, 57, 1723. Safe and efficacious drug candidates remain to be identified from SGLT2 inhibitors, both synthesized and not yet synthesized.